EndothelinA-endothelinB receptor cross-talk and endothelin receptor binding

Abstract

Abstract Background and objective The magnitude of inhibition of an endothelin (ET)-1 response by selective blockade of the ETA or ETB receptors can be limited by apparent compensation mediated by the unblocked receptor. While the mechanism underlying this functionally defined interaction, or ‘cross-talk’, is not clear, binding studies suggest an interaction between the ET receptor subtypes. Key findings These binding studies are reviewed and suggest that, in general, they support the hypothesis that ETA and ETB receptor activation of intracellular signalling pathways influence ET-1 binding to these receptor subtypes. Summary However, the relationship of these binding studies to functional effects and, thus, functional ETA-ETB receptor cross-talk, remains largely untested.